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Regulation Of P-Glycoprotein And Abcp Transporters, Dhanashri Ramkrishna Kolwankar
Regulation Of P-Glycoprotein And Abcp Transporters, Dhanashri Ramkrishna Kolwankar
Graduate Theses, Dissertations, and Problem Reports
The placenta plays an important role in modulating xenobiotic passage from mother to fetus. Smoking is known to induce cytochrome P450 1Al (CYP1A1) expression in the placenta, however its effect on P-glycoprotein (P-gp) and ABC transporter in placenta (ABCP) levels in placenta is not known. In-vitro studies in hepatocytes have reported induction of P-gp mRNA by some polycyclic aromatic hydrocarbons. To examine whether smoking can affect placental P-gp and ABCP, their expression and activity were determined in placentas from smokers and non-smokers. Uptake of [3H]-vinblastine and [3H]-mitoxantrone was used to measure P-gp and ABCP function, respectively and CYP1A1 activity (positive …
Molecular Mechanisms Of G Protein-Receptor Coupling, Janna Eugenievna Slessareva
Molecular Mechanisms Of G Protein-Receptor Coupling, Janna Eugenievna Slessareva
Graduate Theses, Dissertations, and Problem Reports
A big diversity in heterotrimeric G proteins and their cognate receptors raises many questions about the mechanisms that regulate the specificity of signaling along G protein-mediated pathways. The major goal of this project was to understand how the selectivity of G protein-receptor coupling is achieved at the level of the G protein-receptor interface. Additional goals of this project were to assess the generality of molecular mechanisms controlling G protein-receptor coupling selectivity and to investigate how agonist may regulate G protein-receptor interactions. Molecular determinants of G protein-receptor coupling were studied by reconstitution of exogenously supplied, purified G protein heterotrimers with receptors …
Dapsone Activation Of Cyp2c9 Allelic Variants, Matthew Aaron Hummel
Dapsone Activation Of Cyp2c9 Allelic Variants, Matthew Aaron Hummel
Graduate Theses, Dissertations, and Problem Reports
Studies have shown that CYP2C9.1 mediated metabolism of flurbiprofen and naproxen is activated by dapsone. However, dapsone activation has not been studied in the allelic variant forms of CYP2C9. Six concentrations of flurbiprofen or naproxen were co-incubated with six concentrations of dapsone and with reconstituted, purified CYP2C9.1, CYP2C9.2 (R144C), CYP2C9.3 (1359L), or CYP2C9.5 (D360E), in order to assess degrees of activation. Dapsone increased the efficiency (Vmax/Km) of flurbiprofen metabolism 690%, 3029%, 4600%, and 2100% by CYP2C9.1, CYP2C9.2, CYP2C9.3, and CYP2C9.5, respectively. Dapsone increased the efficiency of naproxen metabolism 591%, 1400%, 1150%, and 2100%, by CYP2C9.1, CYP2C9.2, CYP2C9.3, and CYP2C9.5, respectively. …
Molecular Mechanisms Of G Protein-Receptor Coupling, Hongzheng Ma
Molecular Mechanisms Of G Protein-Receptor Coupling, Hongzheng Ma
Graduate Theses, Dissertations, and Problem Reports
A variety of extracellular signals are transmitted into the cell interior by interactions with a superfamily of heptahelical cell surface receptors. Heterotrimeric G proteins mediate the signal transduction by coupling these receptors to intracellular effector proteins. The molecular mechanisms in G protein-receptor coupling processes are still not completely understood. In this project, two aspects of G protein-receptor coupling were examined: (1) the G protein-coupling properties of the five human muscarinic acetylcholine receptors (mAChRs); (2) a novel regulatory mechanism by a newly identified G protein signal regulator, Activator of G-protein Signaling 3 (AGS3). To study the regulation of G protein-receptor coupling, …